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PDBsum entry 3dv1
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References listed in PDB file
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Key reference
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Title
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Macrocyclic peptidomimetic beta-Secretase (bace-1) inhibitors with activity in vivo.
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Authors
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R.Machauer,
K.Laumen,
S.Veenstra,
J.M.Rondeau,
M.Tintelnot-Blomley,
C.Betschart,
A.L.Jaton,
S.Desrayaud,
M.Staufenbiel,
S.Rabe,
P.Paganetti,
U.Neumann.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
1366-1370.
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PubMed id
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Abstract
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The macrocyclic peptidic BACE-1 inhibitors 2a-c show moderate enzymatic and
cellular activity. By exchange of the hydroxyethylene- to
ethanolamine-transition state mimetic the peptidic character was reduced,
providing the highly potent and selective inhibitor 3. Variation of the P'
moiety resulted in the macrocyclic inhibitor 14. Both macrocycles show
inhibition of BACE-1 in the brain of APP51/16 transgenic mice, 3 (NB-544) after
intravenous and 14 (NB-533) after oral application.
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Secondary reference #1
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Title
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Structure-Based design and synthesis of macrocyclic peptidomimetic beta-Secretase (bace-1) inhibitors.
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Authors
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R.Machauer,
S.Veenstra,
J.M.Rondeau,
M.Tintelnot-Blomley,
C.Betschart,
U.Neumann,
P.Paganetti.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
1361-1365.
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PubMed id
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